Clinical Study

Pharmacokinetics of Etravirine Combined with Atazanavir/Ritonavir and a Nucleoside Reverse Transcriptase Inhibitor in Antiretroviral Treatment-Experienced, HIV-1-Infected Patients

Table 2

Pharmacokinetic parameters and statistical analysis of atazanavir after administration of atazanavir/ritonavir 300/100 mg qd for two weeks in combination with two NRTIs (Day −1), followed by administration of etravirine 200 mg bid for two weeks in combination with one NRTI and atazanavir/ritonavir 300/100 mg qd or atazanavir/ritonavir 400/100 mg qd (Week 2).

Pharmacokinetics of atazanavir mean ± SD; : median (range)Group oneGroup two
ATV/r 300/100 mg qd + two NRTIs
(reference)
(*)
ATV/r 300/100 mg qd +
one NRTI + ETR 200 mg bid (Test 1)
()
ATV/r 300/100 mg qd + two NRTIs
(reference)
()
ATV/r 400/100 mg qd + one NRTI + ETR 200 mg bid (Test 2)
()

, ng/mL1339 ± 1728 845.7 ± 703.3 1898 ± 2298 1545 ± 1296
, ng/mL1104 ± 1511 758.6 ± 610.51671 ± 2310 1107 ± 866.8
, ng/mL5652 ± 2735 5232 ± 2166 6419 ± 2853 6950 ± 2693
, h4.00 (1.98–6.00) 3.00 (1.00–4.17) 3.04 (1.00–6.00) 3.21 (1.25–6.17)
, ng⋅h/mL60030 ± 3969055070 ± 21860 74210 ± 5548072220 ± 34600

LSM ratio (90% CI) of test versus reference

0.82 (0.55–1.22)0.91 (0.63–1.33)
0.96 (0.80–1.16)1.05 (0.86–1.27)
0.96 (0.76–1.22)0.99 (0.81–1.21)

ATV/r: atazanavir/ritonavir; : area under the plasma concentration-time curve from time 0 to 24 hours; bid: twice daily; CI: confidence interval; : maximum plasma concentration; : minimum plasma concentration; : predose plasma concentration; ETR: etravirine; LSM: least square mean; NRTI: nucleoside reverse transcriptase inhibitor; qd: once daily; SD: standard deviation; : time to maximum plasma concentration.
* for , for ; for , , and ; for , , and ; for , for ;  calculated based on log-transformed pharmacokinetic parameters.